hP, the component of log P controlling structure-activity relationships amongst non-steroidal anti-inflammatory drugs

被引:1
作者
Dean, FM [1 ]
机构
[1] UNIV LIVERPOOL,DEPT CHEM,LIVERPOOL L69 3BX,MERSEYSIDE,ENGLAND
关键词
D O I
10.1111/j.2042-7158.1996.tb05908.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
A range of 25 drugs and other compounds selected from published sources by strict criteria, has been used to confirm that their ability to inhibit the production of prostaglandin by mouse peritoneal macrophage does not correlate with log P but with hP, the parameter composed of only the hydrophobic contributions (atoms and groups composed of carbon, hydrogen and halogens). Other heteroatoms and physical properties can usually be ignored. Anti-inflammatory activity does not depend upon pK(a) or partition phenomena unless extreme, nor does it depend primarily upon the structural types within the range phenols, salicylic acids, mefenamic acids, areneacetic and profenic acids.
引用
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页码:233 / 239
页数:7
相关论文
共 29 条
[1]  
Akarasereenont Pravit, 1994, British Journal of Pharmacology, V112, p183P
[2]   RATIONALISATIONS AMONG HETEROCYCLIC PARTITION-COEFFICIENTS .3. PI-EXCESSIVE HETEROCYCLES - SOME COMMENTS ON THE CLOGP ALGORITHM [J].
BRADSHAW, J ;
TAYLOR, PJ .
QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIPS, 1989, 8 (04) :279-287
[3]   INHIBITION BY ANTI-INFLAMMATORY DRUGS OF PROSTAGLANDIN PRODUCTION IN CULTURED MACROPHAGES - FACTORS INFLUENCING THE APPARENT DRUG EFFECTS [J].
BRUNE, K ;
RAINSFORD, KD ;
WAGNER, K ;
PESKAR, BA .
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 1981, 315 (03) :269-&
[4]   NOVEL ANTI-INFLAMMATORY AGENTS [J].
CULLEN, E .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1984, 73 (05) :579-589
[5]  
Dearden J C, 1989, Prog Clin Biol Res, V291, P353
[6]   CORRELATION BETWEEN GASTRIC IRRITANCY AND ANTI-INFLAMMATORY ACTIVITY OF NON-STEROIDAL ANTI-INFLAMMATORY DRUGS [J].
DEARDEN, JC ;
NICHOLSON, RM .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1984, 36 (10) :713-715
[7]   STRUCTURE-ACTIVITY-RELATIONSHIPS FOR INHIBITION OF PROSTAGLANDIN CYCLOOXYGENASE BY PHENOLIC-COMPOUNDS [J].
DEWHIRST, FE .
PROSTAGLANDINS, 1980, 20 (02) :209-222
[8]  
FRANKE R, 1984, THEORETICAL DRUG DES
[9]  
GREGG CN, 1991, DISS ABSTR INT, V51, P4290
[10]  
GRENNAN DM, 1986, THERAPEUTICS RHEUMAT, V2, P209